BURLINGTON, Mass. & GRONINGEN, Netherlands—MilliporeSigma and InnoCore Pharmaceuticals have announced a global cooperation agreement to provide InnoCore’s proprietary SynBiosys biodegradable polymer platform. The drug delivery platform can be used to develop sustained-release solutions for biologicals in injectable formulations.

According to Steffen Denzinger, director of strategy and business development, Process Solutions at MilliporeSigma, and Rob Steendam, chief technology officer, InnoCore Pharmaceuticals, “MilliporeSigma’s Actives and Formulations business looks for partners that can help pharmaceutical companies improve their formulations, making them more compliant and improving ease of use to patients. InnoCore Pharmaceuticals was looking for further adoption possibilities for their proprietary technology … it seemed natural to work together using the larger reach of the MilliporeSigma to make this technology even more widely available than InnoCore could have done on its own.

“The technology will be used to help pharmaceutical companies to efficiently develop long-acting, sustained-release solutions for injectables, not only to enhance the release profile and help patient compliance of traditional PLGA formulations, but also especially for large biological drug molecules for which this strategy has been challenging. Together, MilliporeSigma and InnoCore Pharmaceuticals will work closely with future partners to help them efficiently develop such formulations by adapting the technology to their specific biological drug molecules and release pattern needs.”

“Before entering into this collaboration agreement, MilliporeSigma worked with InnoCore Pharmaceuticals on several projects to help progress the further development of the platform technology,” note Denzinger and Steendam. “These projects comprised development of sustained-release microparticle formulations utilizing a variety of biological actives and included both in-vitro and in-vivo studies. Working together to create more data on the performance of the platform technology is still going on, and scientific results will be published in the near future.”

“Until now, formulating large, biological active pharmaceutical ingredients such as proteins and large peptides into long-acting, sustained-release formulations has been difficult, if not impossible,” said Andrew Bulpin, head of Process Solutions at MilliporeSigma. “This collaboration will bring long-acting release of protein therapeutics to market, allowing new and potentially life-changing treatments. It will also improve patient compliance by reducing dosing frequency and maintaining drugs at therapeutic levels longer.”

Sustained-release solutions play an increasingly important role in drug formulation because they enhance patient adherence. The new proprietary technology developed by InnoCore Pharmaceuticals allows the development of injectable sustained-release biological formulations with conserved bioactivity of these sensitive molecules. The SynBiosys platform can be used for subcutaneous, intramuscular and site-specific injectable formulations in the form of microparticles and implants.

Rahael Maladwala, Pharma Analyst at GlobalData, explained, “One of the biggest environmental unmet needs in the pharmaceutical market is a lack of compliance. Indeed, it was estimated that the cost of non-compliance in the U.S. cost the economy somewhere between $100bn and $290bn per year, according to the U.S. National Library of Medicine. Sustained-release drugs for small-molecule drugs are commonplace in the pharmaceutical market; however, this type of technology has not been seen before for biologic molecules, and would increase compliance by reducing the dosing frequency.

“Merck is one of the largest pharmaceutical companies in the world and has a strong pipeline portfolio, with several biologic drugs targeting various different therapy areas, including oncology, cardiovascular, and infectious diseases. If the company can successfully utilize this drug delivery system in the future, their drugs would be at a significant advantage to others on the market and would help fasten their uptake.”

“The beauty of the SynBiosys platform is how versatile it is, and how quickly polymers can be created based on the characteristics of the candidate drug molecule and the target product profile of the final drug delivery product. The proprietary technology combines blocks of biodegradable polymers depending on the drug molecule to be formulated and the desired release kinetics. This versatility allows for screening time efficiency, while more traditional technologies would require more time and effort to synthesize polymers for formulation screening and upscaling after the optimization is achieved,” say Steendam and Denzinger.

“The SynBiosys platform is designed to make the formulator’s life much easier and shorten the time needed to bring a specific formulation to the clinic, making the overall development process more cost-efficient,” they add. “But most importantly, the SynBiosys platform allows the creation of sustained-release formulations for biological drug molecules such as proteins and large peptides which cannot be achieved with the PLGA polymer products marketed currently.”

MilliporeSigma and InnoCore will support customers with formulation, process development and manufacturing services in using this technology to develop injectable sustained-release drug products and overcome formulation challenges—especially for large peptides and proteins. This new, large biomolecule formulation and delivery capability complements MilliporeSigma’s existing portfolio of biodegradable polylactic acid and polylactic glycolic acid (PLA/PLGA) polymers for sustained release in liquid/parenteral formulations. The PLA/PLGA technology applies primarily to small molecules, small hormones and peptides.

“The polylactic and polylactic glycol acids portfolio and the SynBiosys platform are actually complementing each other. PLA/PLGA polymers are already widely used in sustained-release formulation of small molecules and some hormones and peptides nowadays. However, it remains a challenge to efficiently to adapt these delivery systems to the specific needs of larger biologics. Standard PLA/PLGAs can often be problematic in proteins, as upon degradation during the release time locally a lower pH is created that can lead to degradation of the protein,” explain Denzinger and Steendam. “The SynBiosys platform as such may use PLA/PLGA blocks as well together with other hydrophilic polymer blocks, but can be better and quicker adapted to the requirements of larger molecules. MilliporeSigma is now able to support formulators in obtaining the most effective sustained-release solutions for actives of virtually every size and chemical nature.”

“Together we will be able to bring tailor-made injectable sustained-release solutions for virtually every drug molecule API quicker and more efficiently to patients globally. This will make a wider range of actives accessible to patients, and will enable more patient-friendly administration. The most exciting aspect of this collaboration is that this will result in a better quality of life for patients. We are working to help bring life-enhancing drug therapies to market faster,” Steendam and Denzinger conclude.